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Optimization of M(4) positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology

This letter describes the further chemical optimization of the 5-amino-thieno[2,3-c]pyridazine series (VU0467154/VU0467485) of M(4) positive allosteric modulators (PAMs), developed via iterative parallel synthesis, culminating in the discovery of the non-human primate (NHP) in vivo tool compound, VU...

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Bibliographic Details
Published in:Bioorg Med Chem Lett
Main Authors: Melancon, Bruce J., Wood, Michael R., Noetzel, Meredith J., Nance, Kellie D., Engelberg, Eileen M., Han, Changho, Lamsal, Atin, Chang, Sichen, Cho, Hyekyung P., Byers, Frank W., Bubser, Michael, Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Engers, Darren W., Wu, Dedong, Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.
Format: Artigo
Language:Inglês
Published: 2017
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC5508548/
https://ncbi.nlm.nih.gov/pubmed/28442253
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.04.043
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